Five compounds (tenuifoliside C, tenuifoliside D, telephiose A, telephiose C and polygalaxanthone III) from polygala tenuifolia wild were incubated together with CYP probe substrate in human liver microsomes to investigate the inhibitory effect towards CYP450 enzyme. Phenacetin (CYP1A2), coumarin (CYP2A6), paclitaxel (CYP2C8), diclofenac (CYP2C9), S-mepheriytoin (CYP2C19), dextromethorphan (CYP2D6), chlorzoxazone (CYP2E1), midazolam (CYP3A) were selected as the isoforfn specific substrate. And the formation of paracetamol, 7-hydroxycoumarin, 6alpha-hydroxy paclitaxel, 4'-hydroxydiclofenac, dextrorphan, 6-hydroxychlorzoxazone, 1'-hydroxymidazolam, 4'-hydroxymephenytoin were detected respectively to measure the effect towards CYP450 by high-pressure liquid chromatography (HPLC). The result shows that five compounds from polygala tenuifolia willd significantly inhibit chlorzoxazone 6-hydroxylation catalyzed by CYP2E1, while showed no effect towards CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A. And IC50 value was 38.73, 54.14, 61.77, 62.22, 50.56 micromol x L(-1), respectively.
Cytochrome P-450 Enzyme System ; metabolism ; Esters ; pharmacology ; Glycosides ; pharmacology ; Humans ; Microsomes, Liver ; drug effects ; enzymology ; Oligosaccharides ; pharmacology ; Polygala ; chemistry ; Xanthones ; pharmacology

Objective To investigate the level of homocysteine among healthy examination people and the possible related factors.Methods Retrospective analysis was performed to collect 1 259 results of healthy examination people from July to September in 2015,and 564 patients were confirmed to be hyperhomocysteinemia.The serum level of lipoids,glucose,uric acid and blood routine results were also collected.Results The incidence of hyperhomocysteinemia was 45.52％,and man has a higher rate than woman.The results of logistic regression showed positive results of UA (OR =1.006,95％ CI =1.005-1.008),HBG(OR =1.035,95％CI=1.026-1.045),and PLT (OR =0.996,95％ CI =0.993-0.998) in high hyperhomocysteinemia patients.Condusion High UA、HBG and low PLT levels are risk factors in hyperhomocysteinemia,and could be the important way for the early diagnoses of hyperhomocysteinemia.

AIMTo study the effect of the recombined human growth hormone(rhGH) on secretory immunoglobulin A (sIgA), epidermal growth factor (EGF) in rats with obstructive jaundice.

METHODSSixty Wistar rats were randomly divided into four groups, sham-operated (group A), common biliary duct-ligated (group B), biliary duct-ligated plus rhGH-treat for one week (group C), biliary duct-ligated plus rhGH-treat for two weeks (group D), each group had 15 rats. Except group A, the rats of other groups were operated with biliary duct-ligated. Until two weeks after operation, the rats of group A and B were killed. After operation, the rats of group C were treated with rhGH hypodermic injection (0.75 U x kg(-1) x d(-1)) for one week, and then killed. The rats of D group were treated with rhGH hypodermic injection (0.75 U x kg(-1) x d(-1)) for two weeks, and then killed. All procedures were performed aseptically. Total bilirubin (TB), alkaline phosphatase (ALP), prealbumin(PA), insulin-like growth factor (IGF-1), sIgA, EGF were measured.

RESULTSCompared with group A, in group B, C, D, serum level of PA, IGF-1 and sIgA, EGF level of gastric and intestinal juice were lower, but TB, ALP were higher, there were significant difference. Compared with group B, the rats with treatment of rhGH in group C and D had higher sIgA and EGF and lower intestinal bacterial translocation.

CONCLUSIONIn objective jaundice rats, rhGH can protect their hepatic function, intestinal physical-barrier function and immune-barrier function, and reduce intestinal bacterial translocation.

Animals ; Bacterial Translocation ; Epidermal Growth Factor ; metabolism ; Growth Hormone ; pharmacology ; Humans ; Immunoglobulin A, Secretory ; metabolism ; Jaundice, Obstructive ; metabolism ; Rats ; Rats, Wistar ; Recombinant Proteins ; pharmacology

AIMTo investigate the paclitaxel-loaded nanoparticles of poly(ethylene glycol)-b-poly(D,L-lactic acid) amphiphilic diblock copolymer (PMT).

METHODSPMT was prepared by solid dispersion technique. The average size and size distribution were determined by dynamic light scattering (DLS). The morphology was characterized by transmission electron microscopy (TEM) and 1HNMR. The influences of the copolymer molecular weight and the paclitaxel-fed amount on PMT were studied. Therapeutic effect of PMT was studied on Kunming mice liver cancer H22.

RESULTSPMT showed nanometer size and spherical morphology with core and shell. The sizes of PMT increased with increasing the molecular weight of the hydrophobic segment in PEDLLA or increasing the drug-loaded amount. The tumour inhibiting effect of PMT was similar with that of Taxol.

CONCLUSIONIt will provide an experiment basis for the development of new kind of intravenous administration of paclitaxel.

Animals ; Antineoplastic Agents, Phytogenic ; administration & dosage ; pharmacology ; Delayed-Action Preparations ; Drug Carriers ; Drug Delivery Systems ; Lactic Acid ; Liver Neoplasms, Experimental ; pathology ; Mice ; Microspheres ; Nanotechnology ; Paclitaxel ; administration & dosage ; pharmacology ; Particle Size ; Polyethylene Glycols

In order to establish HPLC fingerprint of Liuwei Dihuang soft capsule, and to provide certain reference for an quality control of it, the HPLC method was performed on an Agilent C18 (4.6 mm x 250 mm, 5 μm) column with acetonitrile-0.02% trifluoroacetic acid as mobile phase, gradient elution volume flow of 1.0 mL x min(-1), column temperature was 30 degrees C, detection wavelength: 0-60 min, 238 nm, 60-70 min, 210 nm. The software for chromatographic fingerprint was applied to analysis different batches of Liuwei Dihuang soft capsule samples. Sixteen mutual peaks were selected as the fingerprint peaks in 12 samples with loganin as the reference peak, and all of the detected peaks were separated effectively. Cluster analysis (HCA) and similarity analysis (SA) were done based on data of 12 samples clustering analysis of 12 batches of samples were divided into 2 categories. Including 7 for the first class, the rest was second, similarities calculated by SA were all above 0.92, indicating a good similarity between the reference and twelve batches of samples, also, the analysis results of HCA and SA basically the same. This method is simple with good precision, repeatability and stability, and provides the basis for Liuwei Dihuang soft capsule quality control.
Capsules ; analysis ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Quality Control

This article reports the clinical features and C12orf65 gene mutations of a girl with autosomal recessive spastic paraplegia-55. The 8-year-old girl experienced disease onset at the age of 5 years and had optic atrophy as the main clinical manifestation, with slow movements in standing up and a slight duck-shaped gait. Peripheral blood DNA samples were collected from this child and her parents and brother to perform high-throughput whole-exome sequencing and high-throughput mitochondrial genome sequencing. Sanger sequencing was performed for verification. The results showed two compound heterozygous mutations, c.394C>T and c.447_449delGGAinsGT, in the C12orf65 gene. The former mutation came from her father and was a known pathogenic mutation, and the latter came from her mother and was a novel mutation which had not been reported in literature. This study expands the mutation spectrum of the C12orf65 gene and thus provides a molecular basis for the etiological diagnosis of the child and the genetic counseling of the family.
Child ; Female ; High-Throughput Nucleotide Sequencing ; Humans ; Male ; Mitochondrial Proteins ; genetics ; Mutation ; Pedigree ; Peptide Termination Factors ; genetics ; Spastic Paraplegia, Hereditary ; genetics

Objective:To investigate the clinical characteristics of central nervous system tuberculosis in adults and the possible factors affecting the mortality and disability of the patients.Methods:The clinical data of patients diagnosed as "tuberculous meningitis" "tuberculous meningoencephalitis" "tuberculous cerebrospinal meningitis" or "tuberculous brain ubscess" in Huashan Hospital, Fudan University and Jing′an Branch, Huashan Hospital, Fudan University in Shanghai from January 1, 2010 to December 31, 2017 were collected, and a retrospective cohort was established. The clinical characteristics were analyzed, Medical Research Council (MRC) grade system was used to assess the severity of meningitis, and the modified Rankin Scale was used to assess the impairment of self-care. Survival rate and disability rate of the cohort were analyzed. Binary logistic regression was used for multivariate analysis. Kaplan-Meier survival curve was used for survival analysis.Results:A total of 161 patients with central nervous system tuberculosis were enrolled. Among the 161 patients, 55 cases (34.2%) were confirmed, 72 cases (44.7%) were highly suspected and 34 cases (21.1%) were suspected diagnosis. There were 56 cases (34.8%) with MRC grade Ⅰ, 76 cases (47.2%) with MRC grade Ⅱ and 29 cases (18.0%) patients with MRC grade Ⅲ before treatment. Up to January 1, 2019, ten (6.2%) patients died, 32 (19.9%) patients lost to follow-up, 119 (73.9%) patients survived. The five-year survival rate was 92.83%. There were 72 patients with no impact on life, 34 patients with moderate impact and 13 patients with severe impact. The disability rate was 39.5% (47/119). Binary logistic regression analysis showed that increasing age (odds ratio ( OR)=1.06, 95%confidence interval ( CI) 1.00 to 1.13, P=0.032) and deterioration of MRC grade during anti-tuberculosis treatment ( OR=89.00, 95% CI4.46 to 1 779.00, P=0.003) were independent risk factors for death. When severe disability and death were used as adverse outcomes, logistic regression analysis showed increasing age ( OR=1.07, 95% CI 1.01 to 1.13, P=0.035) and deterioration of MRC grade during anti-tuberculosis treatment ( OR=77.17, 95% CI4.45 to 1 337.00, P=0.003) were still independent risk factors for adverse outcomes. Conclusions:The mortality of central nervous system tuberculosis in adults in this cohort is relatively low, but the disability rate is still high. Increasing age and deterioration of MRC grade during anti-tuberculosis treatment are independent risk factors for death and disability.

OBJECTIVETo measure lutein, zeaxanthin and β-carotene level in foods commonly consumed in Beijing, and compare the content difference between raw and cooked food.

METHODSForty-six commonly consumed foods of 8 classes were collected in Haidian district of Beijing from September to October in 2009. A high performance liquid chromatography method was used to determine the content of lutein, zeaxanthin and β-carotene in both raw and cooked samples.

RESULTSLutein was abundant in cucurbitaceous and solanaceous, allium and nuts, especially in Chinese chive (18 226.9 µg/100 g) and pumpkin (13 265.2 µg/100 g). Major sources of zeaxanthin included round pumpkin, green garlic shoot, corn and eggs, whose level of zeaxanthin were 444.6, 283.5, 279.7, 118.6 - 377.9 µg/100 g, respectively. Zeaxanthin level of those cooked foods changed to 483.9, 239.3, 279.1, 149.5 - 594.7 µg/100 g, respectively. The zeaxanthin level of cooked Chinese chive reached 1081.2 µg/100 g, while we did not detect any zeaxanthin in raw Chinese chive. β-carotene was present in a wide variety of vegetables and fruits. Carrot (17 234.3 µg/100 g) was a good source of β-carotene, while its level in cooked carrot was 17 013.5 µg/100 g.

CONCLUSIONConsuming the proper kinds of foods and changing the method of food processing were beneficial to increase the intake of lutein, zeaxanthin and β-carotene.

China ; Cooking ; Food ; Food Analysis ; Lutein ; analysis ; Xanthophylls ; analysis ; Zeaxanthins ; beta Carotene ; analysis

OBJECTIVETo examine the association of activation of calcium-sensing receptors (CaSR) with apoptosis in cardiomyocytes under simulated ischemia/reperfusion.

METHODSVentricular cardiomyocytes of neonatal rats were incubated in ischemia-mimetic solution for 2 h, then re-incubated in normal culture medium for 24 h to establish a model of simulated ischemia/reperfusion (I/R). Cell apoptosis was detected by terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL assay). The expression of CaSR mRNA was detected by reverse transcriptase polymerase chain reaction (RT-PCR). The expression of Caspase -3 and Bcl-2 was detected by Western blotting.

RESULTThe simulated I/R enhanced the expression of CaSR and cardiomyocyte apoptosis. GdCl(3), a specific activator of CaSR, further increased the expression of CaSR and cardiomyocyte apoptosis, along with upregulation of Caspase-3 and downregulation of Bcl-2.

CONCLUSIONCaSR is associated with I/R injury and apoptosis in neonatal rat ventricular cardiomyocytes via suppressing Bcl-2 and promoting Caspase -3 expression.

Animals ; Apoptosis ; physiology ; Caspase 3 ; metabolism ; Cells, Cultured ; Myocardial Reperfusion Injury ; metabolism ; pathology ; Myocytes, Cardiac ; metabolism ; pathology ; Proto-Oncogene Proteins c-bcl-2 ; metabolism ; Rats ; Receptors, Calcium-Sensing ; metabolism ; Signal Transduction

OBJECTIVETo explore the association of spermatogenic arrest with the expression of estrogen receptor alpha (ERalpha) in human testes.

METHODSWe examined the testicular biopsy specimens of 120 infertile men by HE staining, detected the expression of ERalpha in the specimens of those with spermatogenic arrest by the two-step immunohistochemical method, and compared the results with those of 10 healthy men.

RESULTSOf the 120 specimens from the infertile men, 31 (25.8%) met the diagnostic criteria of spermatogenic arrest. In the testis tissue of normal men, ERalpha expressed in Sertoli, myoid and Leydig cells, but not in spermatogenic cells, while in the testis tissues of those with spermatogenic arrest, ERalpha expressed lowly in Sertoli, myoid and Leydig cells, with statistically significant differences in immunostaining intensity between the two groups (P < 0.05).

CONCLUSIONAndrogen receptor (AR) and ERalpha may play a coordinating role in facilitating spermatogenesis. Spermatogenic arrest may be related to a complex series of disorders in cell signal transduction involving AR, ERalpha and HSP90.

Adult ; Case-Control Studies ; Estrogen Receptor alpha ; metabolism ; Humans ; Infertility, Male ; etiology ; metabolism ; pathology ; Male ; Spermatogenesis ; Testis ; metabolism ; pathology ; Young Adult